Ulixertinib (BVD-523, VRT752271)
Molecular Weight(MW): 433.33
Ulixertinib (BVD-523, VRT752271) is a potent and reversible ERK1/ERK2 inhibitor with IC50 of <0.3 nM for ERK2. Phase 1.
1 Customer Review
Ulixertinib inhibited the proliferation of SUDHL-10 and Raji cells. (A) The activation of ERK1/2 was analyzed by Western blotting. Ulixertinib (0.1, 0.4 and 1.0 nM) significantly inhibited ERK1/2 activation in a dose-dependent manner compared with control cells. Cell proliferation was measured by the CCK-8 assay. Ulixertinib (0.1, 0.4 and 1.0 nM) significantly inhibited proliferation of SUDHL-10 (B) and Raji cells (C) in a time- and dose-dependent manner compared with control cells.
Int J Clin Exp Med, 2016, 9(6):10955-10962.. Ulixertinib (BVD-523, VRT752271) purchased from Selleck.
Purity & Quality Control
Choose Selective ERK Inhibitors
|Description||Ulixertinib (BVD-523, VRT752271) is a potent and reversible ERK1/ERK2 inhibitor with IC50 of <0.3 nM for ERK2. Phase 1.|
In an A375 melanoma cell line containing a b-RAFV600E mutation, Ulixertinib reduces the levels of phosphorylated ERK2 (pERK) and of the phosphorylation of the downstream kinase RSK (pRSK) with IC50 of 4.1/0.14 μM, respectively. Ulixertinib also inhibits A375 cell proliferation with IC50 of 180 nM. 
ERK2 Rapidfire Mass Spectrometry Inhibition of Catalysis Assay:MEK U911-activated ERK2 protein is expressed and purified in-house. Enzyme and substrate solutions are made up in assay buffer consisting of 50 mM Tris (pH 7.5), 10 mM MgCl2, 0.1 mM EGTA, 10 mM DTT and 0.01% (v/v) CHAPS. 1.2 nM ERK2 protein is prepared in assay buffer and 10 µL is dispensed into each well of a polypropylene, 384-well plate containing test and reference control compounds. The compound plates had previously been dosed with a 12 point range from 100 µM down to 0.1 nM in order to calculate compound IC50s, with a total DMSO concentration in the assay of 1%. Following a 20 minute pre-incubation of enzyme and compound at room temperature, 10 µL of substrate solution is added consisting of 16 µM Erktide (IPTTPITTTYFFFK) and 120 µM ATP (measured Km) in assay buffer. The reaction is allowed to progress for 20 minutes at room temperature before being quenched by the addition of 80 µl 1% (v/v) formic acid. The assay plates are then run on the RapidFire Mass Spectrometry platform to measure substrate (unphosphorylated Erktide) and product (phosphorylated Erktide) levels.
|In vitro||DMSO||86 mg/mL (198.46 mM)|
|Ethanol||15 mg/mL (34.61 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03698994||Recruiting||Advanced Malignant Solid Neoplasm|ARAF Gene Mutation|BRAF Gene Mutation|GNA11 Gene Mutation|GNAQ Gene Mutation|HRAS Gene Mutation|KRAS Gene Mutation|MAP2K1 Gene Mutation|MAPK1 Gene Mutation|NF1 Gene Mutation|NRAS Gene Mutation|Recurrent Ependymal Tumor|Recurrent Ewing Sarcoma|Recurrent Glioma|Recurrent Hepatoblastoma|Recurrent Histiocytic and Dendritic Cell Neoplasm|Recurrent Langerhans Cell Histiocytosis|Recurrent Malignant Central Nervous System Neoplasm|Recurrent Malignant Germ Cell Tumor|Recurrent Malignant Solid Neoplasm|Recurrent Medulloblastoma|Recurrent Neuroblastoma|Recurrent Non-Hodgkin Lymphoma|Recurrent Osteosarcoma|Recurrent Peripheral Primitive Neuroectodermal Tumor|Recurrent Rhabdoid Tumor|Recurrent Rhabdomyosarcoma|Recurrent Soft Tissue Sarcoma|Refractory Ependymoma|Refractory Ewing Sarcoma|Refractory Glioma|Refractory Hepatoblastoma|Refractory Histiocytic and Dendritic Cell Neoplasm|Refractory Langerhans Cell Histiocytosis|Refractory Malignant Central Nervous System Neoplasm|Refractory Malignant Germ Cell Tumor|Refractory Malignant Solid Neoplasm|Refractory Medulloblastoma|Refractory Neuroblastoma|Refractory Non-Hodgkin Lymphoma|Refractory Osteosarcoma|Refractory Peripheral Primitive Neuroectodermal Tumor|Refractory Rhabdoid Tumor|Refractory Rhabdomyosarcoma|Refractory Soft Tissue Sarcoma|Wilms Tumor||National Cancer Institute (NCI)||October 1 2018||Phase 2|
|NCT03417739||Recruiting||Uveal Melanoma||Dana-Farber Cancer Institute|BioMed Valley Discoveries Inc||March 26 2018||Phase 2|
|NCT03454035||Recruiting||Tumor Solid|Pancreatic Cancer||UNC Lineberger Comprehensive Cancer Center|BioMed Valley Discoveries Inc|Pfizer||January 30 2018||Phase 1|
|NCT03155620||Recruiting||Advanced Malignant Solid Neoplasm|Ann Arbor Stage III Childhood Non-Hodgkin Lymphoma|Ann Arbor Stage IV Childhood Non-Hodgkin Lymphoma|Childhood Langerhans Cell Histiocytosis|Histiocytic Sarcoma|Juvenile Xanthogranuloma|Malignant Glioma|Recurrent Central Nervous System Neoplasm|Recurrent Childhood Ependymoma|Recurrent Childhood Malignant Germ Cell Tumor|Recurrent Childhood Medulloblastoma|Recurrent Childhood Non-Hodgkin Lymphoma|Recurrent Childhood Rhabdomyosarcoma|Recurrent Childhood Soft Tissue Sarcoma|Recurrent Ewing Sarcoma|Recurrent Glioma|Recurrent Hepatoblastoma|Recurrent Langerhans Cell Histiocytosis|Recurrent Malignant Solid Neoplasm|Recurrent Neuroblastoma|Recurrent Osteosarcoma|Recurrent Peripheral Primitive Neuroectodermal Tumor|Recurrent Rhabdoid Tumor|Refractory Central Nervous System Neoplasm|Refractory Childhood Malignant Germ Cell Tumor|Refractory Ewing Sarcoma|Refractory Glioma|Refractory Hepatoblastoma|Refractory Langerhans Cell Histiocytosis|Refractory Malignant Solid Neoplasm|Refractory Medulloblastoma|Refractory Neuroblastoma|Refractory Non-Hodgkin Lymphoma|Refractory Osteosarcoma|Refractory Peripheral Primitive Neuroectodermal Tumor|Refractory Rhabdoid Tumor|Refractory Rhabdomyosarcoma|Rhabdoid Tumor|Stage III Osteosarcoma AJCC v7|Stage III Soft Tissue Sarcoma AJCC v7|Stage IV Osteosarcoma AJCC v7|Stage IV Soft Tissue Sarcoma AJCC v7|Stage IVA Osteosarcoma AJCC v7|Stage IVB Osteosarcoma AJCC v7|Wilms Tumor||National Cancer Institute (NCI)||July 24 2017||Phase 2|
|NCT02994732||Completed||Healthy||BioMed Valley Discoveries Inc||January 2017||Phase 1|
|NCT02608229||Recruiting||Pancreatic Cancer|Cancer of Pancreas|Cancer of the Pancreas|Pancreas Cancer||Washington University School of Medicine|BioMed Valley Discoveries Inc|National Cancer Institute (NCI)||June 6 2016||Phase 1|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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